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    • 10. 发明申请
    • COMPOSITIONS COMPRISING A PLASMA KALLIKREIN INHIBITOR
    • 包含等离子卡耳列汀抑制剂的组合物
    • WO2017035263A1
    • 2017-03-02
    • PCT/US2016/048456
    • 2016-08-24
    • BIOCRYST PHARMACEUTICALS, INC.
    • BABU, Yarlagadda S.BLOOM, Corey J.BONE, Scott JosephKAUSHAL, Aditya Mohan
    • A61K9/08A61K31/44C07D213/81
    • A61K31/44A61K9/2027A61K9/2054A61K9/2077
    • The present disclosure provides for compositions comprising 3-[2-(4-carbamimidoyl- phenylcarbamoyl)-5-methoxy-4-vinyl-phenyl]-6-(cyclopropylmethyl-carbamoyl)-pyridine-2- carboxylic acid, or a pharmaceutically acceptable form thereof, and a matrix, particularly compositions comprising a solid dispersion or combination of 3-[2-(4-carbamimidoyl- phenylcarbamoyl)-5-methoxy-4-vinyl-phenyl]-6-(cyclopropylmethyl-carbamoyl)-pyridine-2- carboxylic acid, or a pharmaceutically acceptable form thereof, and a concentration enhancing polymer. The compositions provide for higher exposure of 3-[2-(4-carbamimidoyl- phenylcarbamoyl)-5-methoxy-4-vinyl-phenyl]-6-(cyclopropylmethyl-carbamoyl)-pyridine-2- carboxylic acid in the blood for a given dose while at the same time provide for a higher concentration of 3-[2-(4-carbamimidoyl-phenylcarbamoyl)-5-methoxy-4-vinyl-phenyl]-6- (cyclopropylmethyl-carbamoyl)-pyridine-2-carboxylic acid in the blood over time. Dosage forms, dosing protocols and methods of treatment are also provided.
    • 本公开内容提供了包含3- [2-(4-甲脒基 - 苯基氨基甲酰基)-5-甲氧基-4-乙烯基 - 苯基] -6-(环丙基甲基 - 氨基甲酰基) - 吡啶-2-甲酸或其药学上可接受的组合物 特别是包含固体分散体或3- [2-(4-甲脒基 - 苯基氨基甲酰基)-5-甲氧基-4-乙烯基 - 苯基] -6-(环丙基甲基 - 氨基甲酰基) - 吡啶-2-基的组合的组合物, 2-羧酸或其药学上可接受的形式和浓度增强聚合物。 该组合物提供3- [2-(4-甲脒基 - 苯基氨基甲酰基)-5-甲氧基-4-乙烯基 - 苯基] -6-(环丙基甲基 - 氨基甲酰基) - 吡啶-2-甲酸在血液中的较高的暴露量 给定剂量,同时提供更高浓度的3- [2-(4-氨甲酰氨基 - 苯基氨基甲酰基)-5-甲氧基-4-乙烯基 - 苯基] -6-(环丙基甲基 - 氨基甲酰基) - 吡啶-2-甲酸 随着时间的推移,血液中的酸变酸。 还提供了剂量形式,给药方案和治疗方法。